中文摘要：

为了研制一种生物利用度高且具有缓释作用的口服胰岛素制剂，采用静电液滴工艺制备载胰岛素壳聚糖一海藻酸钙微球，以四氧嘧啶为诱导剂建立糖尿病小鼠模型，采用葡萄糖氧化酶法测定小鼠血糖含量，对载药微球的口服药效学进行评价。结果表明：载胰岛素微球平均粒径48μm，药物包封率94．1％，胰岛素相对活性71．7％；药效学研究表明，口服高（4．8IU／kg）、中（3．6IU／kg）、低（2．4IU／kg）3种剂量胰岛素微球，糖尿病小鼠相对血糖值口服6h时降至最低，分别为42．69％，59．8％，76．13％，药理相对生物利用度为41．20％，37．76％，35．81％。口服载胰岛素壳聚糖-海藻酸钠微球具有降血糖作用和显著的缓释作用，药理相对生物利用度高。

英文摘要：

To investigate the hypoglycemic effect of oral insulin-loaded microspheres, a kind of insulin-loaded microspheres was prepared by electrostatic droplet generation with insulin as drug model and alginate combined with chitosan as carrier, diabetic mice was induced by alloxan as animal model, the serum glucose level was determined by GOD-HRP after being orally administrated insulin-loaded microspheres. Experiential results show that main characteristics of microspheres consist of 48 μm average diameter, 94.1% entrapped ratio of insulin and 71.7% relative bioavailability of insulin. The relative serum glucose level of diabetic mice reached the lowest point, i.e. 42.69%, 59.8% and 76.13% respectively after 6 h oral administration with insulin-loaded microspheres dose of 4.8 IU/kg, 3.6 IU/kg and 2.4 IU/kg. The relative pharmacological bioavailability of insulin-loaded microspheres reached 41.20% , 37.76% and 35. 81% after oral administration. The experiment shows that insulin-loaded microspheres has steady and effective hypoglycemic effect after oral administration and the relative pharmacological bioavailability of oral insulin microsphere is higher.